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Amperozide

May 02, 2024

Amperozide is an atypical antipsychotic of the diphenylbutylpiperazine class which acts as an antagonist at the 5-HT2A receptor.[1] It does not block dopamine receptors as with most antipsychotic drugs,[2] but does inhibit dopamine release,[3][4] and alters the firing pattern of dopaminergic neurons.[5] It was investigated for the treatment of schizophrenia in humans,[6] but never adopted clinically. Its main use is instead in veterinary medicine, primarily in intensively farmed pigs, for decreasing aggression and stress and thereby increasing feeding and productivity.[7][8][9]

Amperozide
Clinical data
ATCvet code
Identifiers
  • 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethylpiperazine-1-carboxamide
CAS Number
  • 75558-90-6 Y
PubChem CID
  • 73333
ChemSpider
  • 66062 Y
UNII
  • 0M2W3TAG39
ChEMBL
  • ChEMBL1079935 Y
CompTox Dashboard (EPA)
  • DTXSID6048416
Chemical and physical data
FormulaC23H29F2N3O
Molar mass401.502 g·mol−1
3D model (JSmol)
  • Interactive image
  • CCNC(=O)N1CCN(CC1)CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F
  • InChI=1S/C23H29F2N3O/c1-2-26-23(29)28-16-14-27(15-17-28)13-3-4-22(18-5-9-20(24)10-6-18)19-7-11-21(25)12-8-19/h5-12,22H,2-4,13-17H2,1H3,(H,26,29) Y
  • Key:NNAIYOXJNVGUOM-UHFFFAOYSA-N Y
  (verify)

References edit

  1. ^ Svartengren J, Simonsson P (1990). "Receptor binding properties of amperozide". Pharmacology & Toxicology. 66 (Suppl 1): 8–11. doi:10.1111/j.1600-0773.1990.tb01599.x. PMID 2154737.
  2. ^ Meltzer HY, Zhang Y, Stockmeier CA (May 1992). "Effect of amperozide on rat cortical 5-HT2 and striatal and limbic dopamine D2 receptor occupancy: implications for antipsychotic action". European Journal of Pharmacology. 216 (1): 67–71. doi:10.1016/0014-2999(92)90210-u. PMID 1388121.
  3. ^ Eriksson E (1990). "Amperozide, a putative anti-psychotic drug: uptake inhibition and release of dopamine in vitro in the rat brain". Life Sciences. 47 (23): 2111–7. doi:10.1016/0024-3205(90)90310-n. PMID 1979998.
  4. ^ Yamamoto BK, Meltzer HY (October 1992). "The effect of the atypical antipsychotic drug, amperozide, on carrier-mediated striatal dopamine release measured in vivo". The Journal of Pharmacology and Experimental Therapeutics. 263 (1): 180–5. PMID 1403783.
  5. ^ Grenhoff J, Tung CS, Ugedo L, Svensson TH (1990). "Effects of amperozide, a putative antipsychotic drug, on rat midbrain dopamine neurons recorded in vivo". Pharmacology & Toxicology. 66 (Suppl 1): 29–33. doi:10.1111/j.1600-0773.1990.tb01603.x. PMID 2304893.
  6. ^ Axelsson R, Nilsson A, Christensson E, Björk A (1991). "Effects of amperozide in schizophrenia. An open study of a potent 5-HT2 receptor antagonist". Psychopharmacology. 104 (3): 287–92. doi:10.1007/bf02246025. PMID 1924636. S2CID 2507927.
  7. ^ Kyriakis SC, Martinsson K, Olsson NG, Bjork A (1990). "Thin sow syndrome (TSS): the effect of amperozide". The British Veterinary Journal. 146 (5): 463–7. doi:10.1016/0007-1935(90)90036-3. PMID 2224491.
  8. ^ Kyriakis SC, Olsson NG, Martinsson K, Björk AK (September 1991). "Observations on the action of amperozide: are there social influences on sow-litter productivity?". Research in Veterinary Science. 51 (2): 169–73. doi:10.1016/0034-5288(91)90008-C. PMID 1788479.
  9. ^ Papp I, Waller C, Biro O (October 1996). "[Practical experiences in the therapy of postweaning edema disease in piglets]". Berliner und Munchener Tierarztliche Wochenschrift. 109 (10): 385–7. PMID 8999770.
 

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May 02, 2024
amperozide, atypical, antipsychotic, diphenylbutylpiperazine, class, which, acts, antagonist, ht2a, receptor, does, block, dopamine, receptors, with, most, antipsychotic, drugs, does, inhibit, dopamine, release, alters, firing, pattern, dopaminergic, neurons, . Amperozide is an atypical antipsychotic of the diphenylbutylpiperazine class which acts as an antagonist at the 5 HT2A receptor 1 It does not block dopamine receptors as with most antipsychotic drugs 2 but does inhibit dopamine release 3 4 and alters the firing pattern of dopaminergic neurons 5 It was investigated for the treatment of schizophrenia in humans 6 but never adopted clinically Its main use is instead in veterinary medicine primarily in intensively farmed pigs for decreasing aggression and stress and thereby increasing feeding and productivity 7 8 9 AmperozideClinical dataATCvet codeQN05AX90 WHO IdentifiersIUPAC name 4 4 4 bis 4 fluorophenyl butyl N ethylpiperazine 1 carboxamideCAS Number75558 90 6 YPubChem CID73333ChemSpider66062 YUNII0M2W3TAG39ChEMBLChEMBL1079935 YCompTox Dashboard EPA DTXSID6048416Chemical and physical dataFormulaC 23H 29F 2N 3OMolar mass401 502 g mol 13D model JSmol Interactive imageSMILES CCNC O N1CCN CC1 CCCC C2 CC C C C2 F C3 CC C C C3 FInChI InChI 1S C23H29F2N3O c1 2 26 23 29 28 16 14 27 15 17 28 13 3 4 22 18 5 9 20 24 10 6 18 19 7 11 21 25 12 8 19 h5 12 22H 2 4 13 17H2 1H3 H 26 29 YKey NNAIYOXJNVGUOM UHFFFAOYSA N Y verify References edit Svartengren J Simonsson P 1990 Receptor binding properties of amperozide Pharmacology amp Toxicology 66 Suppl 1 8 11 doi 10 1111 j 1600 0773 1990 tb01599 x PMID 2154737 Meltzer HY Zhang Y Stockmeier CA May 1992 Effect of amperozide on rat cortical 5 HT2 and striatal and limbic dopamine D2 receptor occupancy implications for antipsychotic action European Journal of Pharmacology 216 1 67 71 doi 10 1016 0014 2999 92 90210 u PMID 1388121 Eriksson E 1990 Amperozide a putative anti psychotic drug uptake inhibition and release of dopamine in vitro in the rat brain Life Sciences 47 23 2111 7 doi 10 1016 0024 3205 90 90310 n PMID 1979998 Yamamoto BK Meltzer HY October 1992 The effect of the atypical antipsychotic drug amperozide on carrier mediated striatal dopamine release measured in vivo The Journal of Pharmacology and Experimental Therapeutics 263 1 180 5 PMID 1403783 Grenhoff J Tung CS Ugedo L Svensson TH 1990 Effects of amperozide a putative antipsychotic drug on rat midbrain dopamine neurons recorded in vivo Pharmacology amp Toxicology 66 Suppl 1 29 33 doi 10 1111 j 1600 0773 1990 tb01603 x PMID 2304893 Axelsson R Nilsson A Christensson E Bjork A 1991 Effects of amperozide in schizophrenia An open study of a potent 5 HT2 receptor antagonist Psychopharmacology 104 3 287 92 doi 10 1007 bf02246025 PMID 1924636 S2CID 2507927 Kyriakis SC Martinsson K Olsson NG Bjork A 1990 Thin sow syndrome TSS the effect of amperozide The British Veterinary Journal 146 5 463 7 doi 10 1016 0007 1935 90 90036 3 PMID 2224491 Kyriakis SC Olsson NG Martinsson K Bjork AK September 1991 Observations on the action of amperozide are there social influences on sow litter productivity Research in Veterinary Science 51 2 169 73 doi 10 1016 0034 5288 91 90008 C PMID 1788479 Papp I Waller C Biro O October 1996 Practical experiences in the therapy of postweaning edema disease in piglets Berliner und Munchener Tierarztliche Wochenschrift 109 10 385 7 PMID 8999770 nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Amperozide amp oldid 1194713286, wikipedia, wiki, book, books, library,

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